Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists
作者:Shuwen He、Peter H. Dobbelaar、Jian Liu、Tianying Jian、Iyassu K. Sebhat、Linus S. Lin、Allan Goodman、Cheng Guo、Peter R. Guzzo、Mark Hadden、Alan J. Henderson、Megan Ruenz、Bruce J. Sargent、Larry Yet、Theresa M. Kelly、Oksana Palyha、Yanqing Kan、Jie Pan、Howard Chen、Donald J. Marsh、Lauren P. Shearman、Alison M. Strack、Joseph M. Metzger、Scott D. Feighner、Carina Tan、Andrew D. Howard、Constantin Tamvakopoulos、Qianping Peng、Xiao-Ming Guan、Marc L. Reitman、Arthur A. Patchett、Matthew J. Wyvratt、Ravi P. Nargund
DOI:10.1016/j.bmcl.2010.01.154
日期:2010.3
We report SAR studies on a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead series derived from high-throughput screening hit RY-337. This effort led to the discovery of compound 22e with significantly improved potency at both rodent and human BRS-3. (C) 2010 Elsevier Ltd. All rights reserved.